Cancer chemotherapy with monospecific agents is often hampered by the rapid development of tumor resistance to the drug used. Therefore, combination treatments aiming at several different targets are sought. Viral regulatory proteins, modified or not, appear ideal for this purpose because of their multimodal killing action against neoplastically transformed cells. The large nonstructural protein NS1 of rodent parvoviruses is an excellent candidate for an anticancer agent, shown to interfere specifically with cancer cell growth and survival. The present review describes the structure, functions, and regulation of the multifunctional protein NS1, its specific interference with cell processes and cell protein activities, and what is known so far about the mechanisms underlying NS1 interference with cancer growth. It further outlines prospects for the development of new, multimodal cancer toxins and their potential applications.